N-(pyridin-2-yl)-3-aminocrotonamide

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: N-(pyridin-2-yl)-3-aminocrotonamide
• 英文别名: 3-amino-N-(pyridin-2-yl)crotonamide；N-(pyrid-2-yl)-3-aminocrotonamide；N-(2-pyridyl)-3-aminocrotonamide；(Z)-3-amino-N-pyridin-2-ylbut-2-enamide
• 化学式: C₉H₁₁N₃O
• 分子量: 177.206
• InChiKey: RWUGEDDMAZQWOC-SREVYHEPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  68
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  Ethyl 2-[4'-(3,5-dimethyl-1,2,4-triazol-1-yl)benzoyl]-3-(2'-chlorophenyl)propenoate 、 N-(pyridin-2-yl)-3-aminocrotonamide 在 氮气 、 二乙胺 、 乙酸乙酯 作用下， 以 乙醇 为溶剂， 反应 8.0h， 以to afford the title compound (50 mg, 6%) as a white solid, m.p. 130° C.的产率得到4-(2-chlorophenyl)-1,4-dihydro-2-<4-(3,5-dimethyl-1,2,4-triazol-1-yl)phenyl>-3-(ethoxycarbonyl)-6-methyl-5-pyridine
  参考文献：
  名称：

  Alkyl 2-benzylidene-4-(2-alkylimidazopyrid-1-yl) benzoylacetate esters

  摘要：

  用于合成二氢吡啶血小板活化因子拮抗剂的中间体，其化学式为##STR1##其中R是苯或取代苯; R.sup.3是较低的烷基; Y是1,4-苯撑基，X是2-烷基咪唑吡啶基。

  公开号：

  US05149814A1
• 作为试剂：
  描述：

  N-(pyridin-2-yl)-3-aminocrotonamide 、 2-氯苯甲醛 、 ethyl 4'-(2-methylimidazo<4,5-c>pyrid-1-yl)benzoylacetate 在 N-(pyridin-2-yl)-3-aminocrotonamide 、 2-氯苯甲醛 作用下， 以31的产率得到外消旋-莫地帕泛
  参考文献：
  名称：

  J. Med. Chem. 1992, 35, 3115-3129

  摘要：

  DOI：

文献信息

• Dihydropyridine antiallergic and antiinflammatory agents
  申请人：Pfizer Inc.

  公开号：US04904671A1

  公开（公告）日：1990-02-27

  4-Aryl-2,6-disubstituted-3,5-dicarbamyl-1,4-dihydropyridines and 4-Aryl-2,6-disubstituted-3-alkoxycarbonyl-5-carbamyl-1,4-dihydropyridines as antiallergy and antiinflammatory agents.

  4-芳基-2,6-二取代-3,5-二氨基甲酰基-1,4-二氢吡啶和4-芳基-2,6-二取代-3-烷氧羰基-5-氨基甲酰基-1,4-二氢吡啶作为抗过敏和抗炎药物。
• Alkyl 2-benzylidene-4-(2-alkylimidazopyrid-1-yl) benzoylacetate esters
  申请人：Pfizer Inc

  公开号：US05149814A1

  公开（公告）日：1992-09-22

  Intermediates useful in the synthesis of dihydropyridine platelet activating factor antagonists of the formula ##STR1## where R is phenyl or substituted phenyl; R.sup.3 is lower alkyl; Y is 1,4-phenylene and X is 2-alkylimidazopyridyl.

  用于合成二氢吡啶血小板活化因子拮抗剂的中间体，其化学式为##STR1##其中R是苯或取代苯; R.sup.3是较低的烷基; Y是1,4-苯撑基，X是2-烷基咪唑吡啶基。
• 1,4-dihydro-2-(4-[benzimidazol-l-yl]phenyl)-pyridines as platelet
  申请人：Pfizer Inc.

  公开号：US05063237A1

  公开（公告）日：1991-11-05

  Platelet activating factor antagonists of formula (I): ##STR1## wherein R is phenyl or phenyl substituted by one or more substituents selected from nitro, halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl(C.sub.1 -C.sub.4)alkoxy, fluoro(C.sub.1 -C.sub.4)alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphonyl, hydroxy, trifluoromethyl and cyano, or is phenyl fused to a dioxole ring; R.sup.1 and R.sup.2 are each independently H or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C.sub.1 -C.sub.4 alkyl)piperazinyl or N-(C.sub.2 -C.sub.4 alkanoyl)-piperazinyl group; R.sup.2 is H or C.sub.1 -C.sub.4 alkyl and R.sup.1 is CN, C.sub.3 -C.sub.7 cycloalkyl, aryl, heteroaryl or a C.sub.1 -C.sub.4 alkyl group substituted by one or more substituents selected from C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxycarbonyl, aryl or heteroaryl; Z is selected from C.sub.1 -C.sub.6 alkoxy, aryl(C.sub.1 -C.sub.4)alkoxy, hydroxy, and --NR.sup.4 R.sup.5 wherein each of R.sup.4 and R.sup.5 is independently H or C.sub.1 -C.sub.6 alkyl, or R.sup.4 and R.sup.5 together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl or N-(C.sub.1 -C.sub.4 alkyl)piperazinyl group; Y is 1,4 phenylene or pyridine-2,5-diyl, X is a 5 or 6 membered aromatic heterocyclic group containing one or more nitrogen atoms in its ring; which ring may be fused to a benzene ring or to a further 5- or 6-membered aromatic heterocyclic ring containing one or more nitrogen atoms, at least one of said heterocyclic rings optionally also containing an oxygen or sulphur atom, and being optionally substituted with one or more substituents selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo, CF.sub.3 and CN; and their pharmaceutically acceptable salts.

  公式（I）的血小板活化因子拮抗剂：其中R为苯基或苯基取代物，所述取代物从硝基，卤素，C.sub.1-C.sub.4烷基，C.sub.1-C.sub.4烷氧基，芳基（C.sub.1-C.sub.4）烷氧基，氟代（C.sub.1-C.sub.4）烷氧基，C.sub.1-C.sub.4烷硫基，C.sub.1-C.sub.4烷基磺酰基，羟基，三氟甲基和氰基中选择一个或多个取代；或为融合到二噁英环上的苯基；R.sup.1和R.sup.2各自独立为H或C.sub.1-C.sub.6烷基，或R.sup.1和R.sup.2一起形成吡咯烷基，哌啶基，吗啉基，哌嗪基，N-（C.sub.1-C.sub.4烷基）哌嗪基或N-（C.sub.2-C.sub.4烷酰基）-哌嗪基；其中R.sup.2为H或C.sub.1-C.sub.4烷基，R.sup.1为CN，C.sub.3-C.sub.7环烷基，芳基，杂环芳基或取代一个或多个取代物的C.sub.1-C.sub.4烷基，所述取代物从C.sub.3-C.sub.7环烷基，C.sub.1-C.sub.4烷氧羰基，芳基或杂环芳基中选择一个或多个；Z从C.sub.1-C.sub.6烷氧基，芳基（C.sub.1-C.sub.4）烷氧基，羟基和--NR.sup.4R.sup.5中选择，其中R.sup.4和R.sup.5各自独立为H或C.sub.1-C.sub.6烷基，或R.sup.4和R.sup.5一起形成吡咯烷基，哌啶基，吗啉基，哌嗪基或N-（C.sub.1-C.sub.4烷基）哌嗪基；Y为1,4-苯基或吡啶-2,5-二基，X为含有一个或多个氮原子的5或6元芳香杂环基，其环可以与苯环或另一个含有一个或多个氮原子的5-或6元芳香杂环环融合，所述杂环环中至少有一个可以选择性地含有氧原子或硫原子，并且可以取代一个或多个取代物，所述取代物从C.sub.1-C.sub.4烷基，C.sub.1-C.sub.4烷氧基，卤素，CF.sub.3和CN中选择一个或多个；以及其医药上可接受的盐。
• Alkyl 2-benzylidene-4-(benzimidazol-1-yl) benzoylacetate esters as
  申请人：Pfizer Inc.

  公开号：US05070205A1

  公开（公告）日：1991-12-03

  Intermediates useful in the synthesis of dihydropyridine platelet activating factor antagonists of the formula ##STR1## where R is phenyl or substituted phenyl; R.sup.3 is lower alkyl; Y is 1,4-phenylene and X is a benzimidazol-1-yl.

  在合成二氢吡啶血小板活化因子拮抗剂的中间体中有用的化合物的化学式如下：##STR1## 其中R为苯基或取代苯基；R.sup.3为低碳基；Y为1,4-苯基；X为苯并咪唑-1-基。
• Dihydropyridine anti-allergic and anti-inflammatory agents
  申请人：Pfizer Inc.

  公开号：US04859686A1

  公开（公告）日：1989-08-22

  4-Aryl-3-alkoxycarbonyl-6-methyl-5-carbamyl-2-triazolylalkoxymethyl-1,4-dih yd ropyridines as anti-allergic and anti-inflammatory agents.

  4-芳基-3-烷氧羰基-6-甲基-5-氨基甲酰基-2-三唑基烷氧甲基-1,4-二氢吡啶是抗过敏和抗炎药物。